Syntheses and complement inhibitory activities of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids.

doi:10.1021/JM00380A002

Paper

Syntheses and complement inhibitory activities of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids.

Published Feb 1, 1985 · D. M. Bailey, G. Degrazia, E. J. Alexander

Journal of medicinal chemistry

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5

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Abstract

The syntheses of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids are described. These compounds express potent in vitro inhibition of the human classical complement pathway, and qualitative SAR have been determined. Several of the in vitro active compounds also suppressed the complement dependent reverse passive Arthus reaction (RPAR) in guinea pigs.

Study Snapshot

4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids show potent complement inhibitory activities and suppress the complement-dependent reverse passive Arthus reaction in guinea pigs.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Syntheses and complement inhibitory activities of 4-(2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids.

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References

Citations

A synthetic 2,3-diarylindole induces cell death via apoptosis and autophagy in A549 lung cancer cells.

The synthetic 2,3-diarylindole PCNT13 effectively induces cell death in A549 lung cancer cells through apoptosis and autophagy.

Palladium-catalyzed direct arylation of indoles with cyclohexanones.

This novel palladium-catalyzed method for 3-arylindoles from indoles and cyclohexanones shows good regioselectivity and affords 3-arylindoles as the sole products.

Synthetic peptide inhibitors of complement serine proteases--II. Effects on hemolytic activity and production of C3a and C4a.

Synthetic peptides based on antithrombin III are more effective in inhibiting hemolysis, potentially by inhibiting enzymes other than C1s and C4b2a in the classical pathway and C3bBb in the alternative pathway.

Synthetic peptide inhibitors of complement serine proteases--III. Significant increase in inhibitor potency provides further support for the functional equivalence hypothesis.

Synthetic peptide inhibitors of complement serine proteases--III show significant increase in inhibitor potency, supporting the functional equivalence hypothesis.